Document Report Card

ID: ALA1149343

Journal: J Med Chem

Title: Discovery of antiglioma activity of biaryl 1,2,3,4-tetrahydroisoquinoline derivatives and conformationally flexible analogues.

Authors: Mohler ML, Kang GS, Hong SS, Patil R, Kirichenko OV, Li W, Rakov IM, Geisert EE, Miller DD.

Abstract: Cultured rat astrocytes and C6 rat glioma were used as a differential screen for a variety of 1,2,3,4-tetrahydroisoquinoline (THI) derivatives. Compound 1 [1-(biphenyl-4-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol hydrochloride] selectively blocked the growth of C6 glioma leaving normal astrocytes relatively unaffected. The potential for clinical utility of 1 was further substantiated in human gliomas and other tumor cell lines. Preliminary SAR of this activity was characterized by synthesis and testing of several THI and conformationally flexible variants.

CiteXplore: 16970409

DOI: 10.1021/jm060020x